eplerenone (Rx)

Brand and Other Names:Inspra
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 25mg
  • 50mg
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Hypertension (HTN)

Initial 50 mg PO qDay; may increase to 50 mg PO q12hr; may take up to four weeks for full therapeutic response; hyperkelemia may occur with doses >100 mg/day

Heart Failure Post MI

Initial 25 mg PO qDay; may titrate to maximum of 50 mg once daily within 4 weeks as tolerated

Dose adjustments may be required based on potassium levels

Renal Impairment

Contraindicated if CrCl <50 mL/min or serum creatinine >2 mg/dL in males or >1.8 mg/dL in females

Hepatic Impairment

Dose adjustment not necessary

Dosing considerations

In post-MI CHF patients taking a moderate CYP3A inhibitor, do not exceed 25 mg once daily; in patients with hypertension taking a moderate CYP3A inhibitor, initiate at 25 mg once daily; for inadequate blood pressure response, dosing may be increased to a maximum of 25 mg twice daily

Other Indications and Uses

Improving survival of stable patients with LV systolic dysfunction (LVEF ≤40%) and CHF after an acute myocardial infarction (MI)

Safety and efficacy not established

Hypertension

Initial 50 mg PO qDay; may increase to 50 mg PO q12hr; may take up to four weeks for full therapeutic response; hyperkelemia may occur with doses >100 mg/day

Heart Failure Post MI

Initial 25 mg PO qDay; may titrate to maximum of 50 mg once daily within 4 weeks as tolerated

Dose adjustments may be required based on potassium levels

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Interactions

Interaction Checker

and eplerenone

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            1-10%

            Hyperkalemia (2-10%)

            Increased risk of hyperkalemia with presence of renal dysfunction

            1-3%

            • Dizziness
            • Fatigue/malaise
            • Abdominal pain
            • Diarrhea
            • Albuminuria
            • Hypercholesterolemia
            • Hypertriglyceridemia
            • Cough

            <1%

            Abnormal vaginal bleeding

            Gynecomastia

            Mastodynia

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            Warnings

            Contraindications

            Hypersensitivity

            For all patients: Serum potassium >5.5 mEq/L at initiation Creatinine clearance ≤30 mL/min Concomitant use with strong CYP3A inhibitors For the treatment of hypertension: Type 2 diabetes with microalbuminuria Serum creatinine >2.0 mg/dL in males, >1.8 mg/dL in females Creatinine clearance <50 mL/min Concomitant use of potassium supplements or potassium-sparing diuretics

            For all patients

            • Serum potassium >5.5 mEq/L at initiation
            • Creatinine clearance ≤30 mL/min
            • Concomitant use with strong CYP3A inhibitors

            For the treatment of hypertension

            • Type 2 diabetes with microalbuminuria
            • Serum creatinine >2.0 mg/dL in males, >1.8 mg/dL in females
            • Creatinine clearance <50 mL/min
            • Concomitant use of potassium supplements or potassium-sparing diuretics

            Cautions

            Hyperkalemia, liver dysfunction, metabolic or respiratory acidosis, renal impairment, hypersensitivity to spironolactone

            The risk of hyperkalemia is higher in patients with impaired renal function, proteinuria , diabetes and those concomitantly treated with ACEs, ARBs, NSAIDs and moderate CYP3A inhibitors

            Patients taking moderate CYP3A inhibitors that cannot be avoided should have their dose of eplerenone reduced

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            Pregnancy & Lactation

            Pregnancy

            Available data from published case reports on eplerenone use during pregnancy are insufficient to establish a drug-associated risk of major birth defects, miscarriage, adverse maternal or fetal outcomes; in animal studies, no adverse developmental effects were observed when eplerenone was administered to pregnant rats and rabbits during organogenesis at exposures 32 and 31 times, respectively the human exposure at the 100 mg/day therapeutic dose

            Hypertension in pregnancy increases maternal risk for pre-eclampsia, gestational diabetes, premature delivery, and delivery complications (e.g., need for cesarean section, and post-partum hemorrhage); hypertension increases fetal risk for intrauterine growth restriction and intrauterine death; pregnant women with hypertension should be carefully monitored and managed accordingly

            Infertility

            • Based on animal data, therapy may compromise male fertility; in mature rates, male fertility was decreased with eplerenone exposure at 17 times the 100 mg/day human therapeutic dose; reversibility of effect, not evaluated

            Lactation

            There are no human data available on whether eplerenone is present in human milk, or has effects on breastfed infants or on milk production; eplerenone was present in milk of lactating rats; when a drug is present in animal milk, it is likely that the drug will be present in human milk

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Selective aldosterone receptor antagonist; blocks aldosterone binding at the mineralocorticoid receptor

            Pharmacokinetics

            Half-Life: 3.5-6 hr

            Peak Plasma Time: 1-2 hr

            Bioavailability: 69%

            Protein Bound: 50%

            Vd: 43-90 L

            Metabolism: primarily hepatic CYP3A4

            Metabolite: no active mets identified

            Total Body Clearance: 10 L/hr

            Excretion: feces (32%) and urine (67%)

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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
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            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
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            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.